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Hyrtiosal, a PTP1B Inhibitor from the Marine Sponge Hyrtios erectus , Shows Extensive Cellular Effects on PI3K/AKT Activation, Glucose Transport, and TGFβ/Smad2 Signaling by Tao Sun; Qi Wang; Zhiguo Yu; Yu Zhang; Yuewei Guo; Kaixian Chen; Xu Shen; Hualiang Jiang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Hyrtiosal, a PTP1B Inhibitor from the Marine Sponge Hyrtios erectus , Shows Extensive Cellular Effects on PI3K/AKT Activation, Glucose Transport, and TGFβ/Smad2 Signaling about?
## Abstract Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling, and PTP1B inhibitors have been seen as promising therapeutic agents against obesity and type 2 diabetes. Here we report that the marine natural product hyrtiosal, from the marine sponge __Hyrtios erectus__, has been discovered to act as a PTP1B inhibitor and to show extensive cellular effects on PI3K/AKT activation, glucose transport, and TGFβ/Smad2 signaling. This inhibitor wad able to inhibit PTP1B activity in dose‐dependent fashion, with an IC~50~ value of 42 μM in a noncompetitive inhibition mode. Further study with an IN Cell Analyzer 1000 cellular fluorescence imaging instrument showed that hyrtiosal displayed potent activity in abolishing the retardation of AKT membrane translocation caused by PTP1B overexpression in CHO cells. Moreover, it was found that this newly identified PTP1B inhibitor could dramatically enhance the membrane translocation of the key glucose transporter Glut4 in PTP1B‐overexpressed CHO cells. Additionally, in view of our recent finding that PTP1B was able to modulate insulin‐mediated inhibition of Smad2 activation, hyrtiosal was also tested for its capabilities
Who reads Hyrtiosal, a PTP1B Inhibitor from the Marine Sponge Hyrtios erectus , Shows Extensive Cellular Effects on PI3K/AKT Activation, Glucose Transport, and TGFβ/Smad2 Signaling?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Tao Sun; Qi Wang; Zhiguo Yu; Yu Zhang; Yuewei Guo; Kaixian Chen; Xu Shen; Hualiang Jiang
- Publisher
- Wiley
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)